CN105555786A

CN105555786A - 作为BET蛋白和极体样激酶的双重抑制剂的取代的二氢吡啶并[3,4-b]吡嗪酮

作为BET蛋白和极体样激酶的双重抑制剂的取代的二氢吡啶并[3,4-b]吡嗪酮 Download PDF

Info

Publication number: CN105555786A
Authority: CN; China
Prior art keywords: alkyl; represent; methyl; group; optionally
Prior art date: 2013-07-23
Legal status : Pending

Application number

CN201480052256.5A

Other languages

English (en)

Chinese (zh)

Inventor

N.施梅斯

B.巴德

B.亨德勒

V.舒尔策

I.哈通

N.伯恩克

F.皮勒

Current Assignee

Bayer Pharma AG

Original Assignee

Bayer Pharma AG

Priority date

2013-07-23

Filing date

2014-07-21

Publication date

2016-05-04

2014-07-21 Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG

2016-05-04 Publication of CN105555786A publication Critical patent/CN105555786A/zh

Status Pending legal-status Critical Current

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239000003112 inhibitor Substances 0.000 title abstract description 33
101000582926 Dictyostelium discoideum Probable serine/threonine-protein kinase PLK Proteins 0.000 title abstract description 3
230000009977 dual effect Effects 0.000 title abstract description 3
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150000001875 compounds Chemical class 0.000 claims abstract description 219
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 35
238000002360 preparation method Methods 0.000 claims abstract description 31
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-1 2-C 4-thiazolinyl- Chemical group 0.000 claims description 274
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 98
125000004043 oxo group Chemical group O=* 0.000 claims description 59
229910052739 hydrogen Inorganic materials 0.000 claims description 57
239000001257 hydrogen Substances 0.000 claims description 57
239000011570 nicotinamide Substances 0.000 claims description 52
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 51
125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 49
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GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims description 31
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201000010099 disease Diseases 0.000 claims description 28
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 27
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KQYKBNQFAINVQE-UHFFFAOYSA-N 2h-pyrido[3,4-b]pyrazin-3-one Chemical compound C1=CN=CC2=NC(=O)CN=C21 KQYKBNQFAINVQE-UHFFFAOYSA-N 0.000 claims description 18
229910052799 carbon Inorganic materials 0.000 claims description 18
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